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Potent, Selective, and Cell Active Protein Arginine Methyltransferase 5 (PRMT5) Inhibitor Developed by Structure-Based Virtual Screening and Hit Optimization.

Shandong University
Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6.

Icahn School of Medicine At Mount Sinai
Discovery of a Potent Class I Protein Arginine Methyltransferase Fragment Inhibitor.

University of Toronto
Discovery and structure-activity analysis of 4-((5-nitropyrimidin-4-yl)amino)benzimidamide derivatives as novel protein arginine methyltransferase 1 (PRMT1) inhibitors.

Sichuan University
Selective inhibitors of protein methyltransferases.

Icahn School of Medicine At Mount Sinai
Exploration of cyanine compounds as selective inhibitors of protein arginine methyltransferases: synthesis and biological evaluation.

The University of Georgia
Diamidine compounds for selective inhibition of protein arginine methyltransferase 1.

The University of Georgia
A medicinal chemistry perspective for targeting histone H3 lysine-79 methyltransferase DOT1L.

Baylor College of Medicine
Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.

TBA
Synthesis and structure-activity relationship investigation of adenosine-containing inhibitors of histone methyltransferase DOT1L.

Baylor College of Medicine
Oncoepigenomics: making histone lysine methylation count.

TBA
Synthesis and evaluation of carbocyanine dyes as PRMT inhibitors and imaging agents.

Georgia State University
Pyrazole inhibitors of coactivator associated arginine methyltransferase 1 (CARM1).

Bristol-Myers Squibb Pharmaceutical Research and Development
Novel 3,5-bis(bromohydroxybenzylidene)piperidin-4-ones as coactivator-associated arginine methyltransferase 1 inhibitors: enzyme selectivity and cellular activity.

The University of Texas M.D. Anderson Cancer Center
Discovery and mechanistic study of a class of protein arginine methylation inhibitors.

Georgia State University
1,2-Diamines as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1).

Methylgene
Benzo[d]imidazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)--Hit to Lead studies.

Bristol-Myers Squibb Pharmaceutical Research and Development
Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1).

Bristol-Myers Squibb Pharmaceutical Research and Development
Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia.

University of Cambridge
NVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family.

Johann Wolfgang Goethe University
Novel orally bioavailable EZH1/2 dual inhibitors with greater antitumor efficacy than an EZH2 selective inhibitor.

Daiichi Sankyo Co., Ltd
Development of selective class I protein arginine methyltransferase inhibitors through fragment-based drug design approach.

CSIR-Indian Institute of Chemical Biology (IICB)
Discovery of tetrahydroisoquinolineindole derivatives as first dual PRMT5 inhibitors/hnRNP E1 upregulators: Design, synthesis and biological evaluation.

University of Jinan
Discovery of a Highly Potent and Selective Inhibitor Targeting Protein Lysine Methyltransferase NSD2.

Sun Yat-Sen University
An Adenosine Analogue Library Reveals Insights into Active Sites of Protein Arginine Methyltransferases and Enables the Discovery of a Selective PRMT4 Inhibitor.

Purdue University
Discovery of a Highly Potent Lysine Methyltransferases G9a/NSD2 Dual Inhibitor to Treat Solid Tumors.

Sun Yat-Sen University
Development of (2-(Benzyloxy)phenyl)methanamine Derivatives as Potent and Selective Inhibitors of CARM1 for the Treatment of Melanoma.

Zhejiang Sci-Tech University
Structure-based discovery of a new series of nucleoside-derived ring-opening PRMT5 inhibitors.

University of Chinese Academy of Sciences
A CARM1 Inhibitor Potently Suppresses Breast Cancer Both In Vitro and In Vivo.

Xiamen University
Discovery of potent small molecule inhibitors of histone lysine methyltransferase NSDs.

Jiangsu University of Technology
Overview of the development of protein arginine methyltransferase modulators: Achievements and future directions.

China Pharmaceutical University
Small molecules targeting selected histone methyltransferases (HMTs) for cancer treatment: Current progress and novel strategies.

First Affiliated Hospital of Gannan Medical University
Synthesis and biological evaluation of 1-phenyl-tetrahydro-β-carboline-based first dual PRMT5/EGFR inhibitors as potential anticancer agents.

Shandong University
Structure-based discovery of potent CARM1 inhibitors for colorectal cancer therapy.

East China Normal University
Identification of a Protein Arginine Methyltransferase 7 (PRMT7)/Protein Arginine Methyltransferase 9 (PRMT9) Inhibitor.

University of Salerno
Structure-Based Design and Characterization of the Highly Potent and Selective Covalent Inhibitors Targeting the Lysine Methyltransferases G9a/GLP.

Sun Yat-Sen University
Discovery of a New-Generation S-Adenosylmethionine-Noncompetitive Covalent Inhibitor Targeting the Lysine Methyltransferase Enhancer of Zeste Homologue 2.

Sun Yat-Sen University
Discovery of cysteine-targeting covalent histone methyltransferase inhibitors.

Nanjing Medical University
Structural Modification and Pharmacological Evaluation of Substituted Quinoline-5,8-diones as Potent NSD2 Inhibitors.

Shanghai Jiao Tong University
Medicinal chemistry strategies targeting PRMT5 for cancer therapy.

Sichuan University
Structure-Based Discovery of Potent CARM1 Inhibitors for Solid Tumor and Cancer Immunology Therapy.

Shanghai Institute of Materia Medica
Structure-Aided Design, Synthesis, and Biological Evaluation of Potent and Selective Non-Nucleoside Inhibitors Targeting Protein Arginine Methyltransferase 5.

Sun Yat-Sen University
Turning Nonselective Inhibitors of Type I Protein Arginine Methyltransferases into Potent and Selective Inhibitors of Protein Arginine Methyltransferase 4 through a Deconstruction-Reconstruction and Fragment-Growing Approach.

Institut De G£N£Tique Et De Biologie Mol£Culaire Et Cellulaire
Fascinating Transformation of SAM-Competitive Protein Methyltransferase Inhibitors from Nucleoside Analogues to Non-Nucleoside Analogues.

Csir-Indian Institute of Chemical Biology
A First-in-Class, Highly Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 6.

Icahn School of Medicine At Mount Sinai
5-Aminonaphthalene derivatives as selective nonnucleoside nuclear receptor binding SET domain-protein 2 (NSD2) inhibitors for the treatment of multiple myeloma.

Chinese Academy of Sciences
Pharmacophore-based screening of diamidine small molecule inhibitors for protein arginine methyltransferases.

University of Georgia
Discovery of a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor by Virtual Screening.

University of Toronto
Discovery of 2-substituted-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-1,2,3,4-tetrahydroisoquinoline-6-carboxamide as potent and selective protein arginine methyltransferases 5 inhibitors: Design, synthesis and biological evaluation.

Shanghai Institute of Materia Medica
Histone methyl transferases: A class of epigenetic opportunities to counter uncontrolled cell proliferation.

Punjabi University
Design and Synthesis of Potent, Selective Inhibitors of Protein Arginine Methyltransferase 4 against Acute Myeloid Leukemia.

Chinese Academy of Sciences
Discovery of a First-in-Class Protein Arginine Methyltransferase 6 (PRMT6) Covalent Inhibitor.

Icahn School of Medicine At Mount Sinai
Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors.

University of Jinan
Synthesis, Activity and Metabolic Stability of Non-Ribose Containing Inhibitors of Histone Methyltransferase DOT1L.

Baylor College of Medicine
Identification of a novel selective small-molecule inhibitor of protein arginine methyltransferase 5 (PRMT5) by virtual screening, resynthesis and biological evaluations.

University of Jinan
Development of Potent Type I Protein Arginine Methyltransferase (PRMT) Inhibitors of Leukemia Cell Proliferation.

Zhejiang Sci-Tech University
Method of increasing platelet counts of a subject

Korea Basic Science Institute
Amide-substituted heterocyclic compounds useful as modulators of IL-12, IL-23 and/or IFN alpha responses

Bristol-Myers Squibb
Compounds for the treatment of pain

Alkermes
Tricyclic heterocycles as BET protein inhibitors

Incyte
Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes

Merck Sharpe & Dohme
Androstane and pregnane steroids with potent allosteric GABA receptor chloride ionophore modulating properties

Research Triangle Institute
Cloning, expression, and pharmacological characterization of a novel human histamine receptor.

Smithkline Beecham Pharmaceuticals